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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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Purity: ≥98%
Raltegravir potassium (formerly also known as MK-0518 potassium; trade name: Isentress) is a novel, potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. Raltegravir is an antiretroviral drug used to treat HIV infection. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication. It is the first integrase inhibitors that received FDA approval for HIV treatment.
| ln Vitro |
PFV IN with the S217H alteration has an IC50 of 900 nM, making it ten times less sensitive to raltegravir. PFV IN exhibited 10% of WT's activity and was inhibited by Raltegravir at an IC50 of 200 nM, suggesting that PFV IN is less sensitive to IN strand transfer inhibitors (INSTIs) than WT IN is. Similar to the WT enzyme, S217Q PFV IN is also susceptible to raltegravir [1]. Glucuronidation, not the liver, is the mechanism of raltegravir metabolism. With a 95% inhibitory concentration of 31±20 nM in human T cell cultures, raltegravir demonstrates strong anti-HIV-1 action in vitro. Raltegravir exhibited anti-HIV-2 activity in CEMx174 cells as well, with an IC95 of 6 nM. Glucuronidation is the main mechanism of raltegravir metabolism. Strong glucuronidase UGT1A1 inducers should not be utilized since they drastically lower raltegravir concentrations. Hepatic cytochrome P450 activity is only slightly inhibited by raltegravir. Neither CYP3A4-dependent testosterone 6-beta-hydroxylase activity nor CYP3A4 RNA expression are induced by raltegravir [2]. Magnesium and calcium have been shown to decrease raltegravir's cellular permeability [3]. Effectively preventing viral replication is possible with raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs) [4]. Latisavue successfully suppressed SIVmac251 replication in the acutely infected human lymphoid CD4+ T cell lines MT-4 and CEMx174, suggesting an EC90 in the low nanomolar range [5].
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| ln Vivo |
Rateltelevir improves the viro-immunological status of nonhuman primates infected with SIVmac251 as it progresses. Raltegravir monotherapy results in an undetectable viral load in one non-human primate[5].
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| Additional Infomation |
Raltegravir (brand names: Isentress and Isentress HD) is a prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of HIV infection in adults and children. One form of raltegravir, Isentress, is approved for adults and children weighing at least 4 lb and 4 oz (2 kg). Another form of raltegravir, Isentress HD, is approved for adults and children weighing at least 88 lb (40 kg). Raltegravir is always used in combination with other HIV medicines.
Raltegravir Potassium is the orally bioavailable potassium salt of a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI) with HIV-1 antiviral activity. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication. A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION. See also: Raltegravir (has active moiety); Lamivudine; raltegravir potassium (component of). Drug Indication Isentress is indicated in combination with other anti-retroviral medicinal products for the treatment of human immunodeficiency virus (HIV 1) infection. |
| Molecular Formula |
C20H20FKN6O5
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|---|---|
| Molecular Weight |
482.51
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| Exact Mass |
482.111
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| CAS # |
871038-72-1
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| Related CAS # |
Raltegravir;518048-05-0;Raltegravir-d3 potassium;1246816-98-7;Raltegravir sodium;1292804-07-9
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| PubChem CID |
23668479
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| Appearance |
White to off-white solid powder
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| Density |
1.46 g/cm3
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| Melting Point |
282ºC
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| LogP |
2.131
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
843
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IFUKBHBISRAZTF-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C20H21FN6O5.K/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11;/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30);/q;+1/p-1
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| Chemical Name |
potassium;4-[(4-fluorophenyl)methylcarbamoyl]-1-methyl-2-[2-[(5-methyl-1,3,4-oxadiazole-2-carbonyl)amino]propan-2-yl]-6-oxopyrimidin-5-olate
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| Synonyms |
MK-0518; MK0518; MK 0518; MK-0518 potassium; Raltegravir; trade name: Isentress
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30 mg/mL Solubility in Formulation 5: 25 mg/mL (51.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0725 mL | 10.3625 mL | 20.7250 mL | |
| 5 mM | 0.4145 mL | 2.0725 mL | 4.1450 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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